GLPBio

Apoptosis

Read More about this category

As one of the cellular death mechanisms, apoptosis, also known as programmed cell death, can be defined as the process of a proper death of any cell under certain or necessary conditions. Apoptosis is controlled by the interactions between several molecules and responsible for the elimination of unwanted cells from the body.

Many biochemical events and a series of morphological changes occur at the early stage and increasingly continue till the end of apoptosis process. Morphological event cascade including cytoplasmic filament aggregation, nuclear condensation, cellular fragmentation, and plasma membrane blebbing finally results in the formation of apoptotic bodies. Several biochemical changes such as protein modifications/degradations, DNA and chromatin deteriorations, and synthesis of cell surface markers form morphological process during apoptosis.

Apoptosis can be stimulated by two different pathways: (1) intrinsic pathway (or mitochondria pathway) that mainly occurs via release of cytochrome c from the mitochondria and (2) extrinsic pathway when Fas death receptor is activated by a signal coming from the outside of the cell.

Different gene families such as caspases, inhibitor of apoptosis proteins, B cell lymphoma (Bcl)-2 family, tumor necrosis factor (TNF) receptor gene superfamily, or p53 gene are involved and/or collaborate in the process of apoptosis.

Caspase family comprises conserved cysteine aspartic-specific proteases, and members of caspase family are considerably crucial in the regulation of apoptosis. There are 14 different caspases in mammals, and they are basically classified as the initiators including caspase-2, -8, -9, and -10; and the effectors including caspase-3, -6, -7, and -14; and also the cytokine activators including caspase-1, -4, -5, -11, -12, and -13. In vertebrates, caspase-dependent apoptosis occurs through two main interconnected pathways which are intrinsic and extrinsic pathways. The intrinsic or mitochondrial apoptosis pathway can be activated through various cellular stresses that lead to cytochrome c release from the mitochondria and the formation of the apoptosome, comprised of APAF1, cytochrome c, ATP, and caspase-9, resulting in the activation of caspase-9. Active caspase-9 then initiates apoptosis by cleaving and thereby activating executioner caspases. The extrinsic apoptosis pathway is activated through the binding of a ligand to a death receptor, which in turn leads, with the help of the adapter proteins (FADD/TRADD), to recruitment, dimerization, and activation of caspase-8 (or 10). Active caspase-8 (or 10) then either initiates apoptosis directly by cleaving and thereby activating executioner caspase (-3, -6, -7), or activates the intrinsic apoptotic pathway through cleavage of BID to induce efficient cell death. In a heat shock-induced death, caspase-2 induces apoptosis via cleavage of Bid.

Bcl-2 family members are divided into three subfamilies including (i) pro-survival subfamily members (Bcl-2, Bcl-xl, Bcl-W, MCL1, and BFL1/A1), (ii) BH3-only subfamily members (Bad, Bim, Noxa, and Puma9), and (iii) pro-apoptotic mediator subfamily members (Bax and Bak). Following activation of the intrinsic pathway by cellular stress, pro‑apoptotic BCL‑2 homology 3 (BH3)‑only proteins inhibit the anti‑apoptotic proteins Bcl‑2, Bcl-xl, Bcl‑W and MCL1. The subsequent activation and oligomerization of the Bak and Bax result in mitochondrial outer membrane permeabilization (MOMP). This results in the release of cytochrome c and SMAC from the mitochondria. Cytochrome c forms a complex with caspase-9 and APAF1, which leads to the activation of caspase-9. Caspase-9 then activates caspase-3 and caspase-7, resulting in cell death. Inhibition of this process by anti‑apoptotic Bcl‑2 proteins occurs via sequestration of pro‑apoptotic proteins through binding to their BH3 motifs.

One of the most important ways of triggering apoptosis is mediated through death receptors (DRs), which are classified in TNF superfamily. There exist six DRs: DR1 (also called TNFR1); DR2 (also called Fas); DR3, to which VEGI binds; DR4 and DR5, to which TRAIL binds; and DR6, no ligand has yet been identified that binds to DR6. The induction of apoptosis by TNF ligands is initiated by binding to their specific DRs, such as TNFα/TNFR1, FasL /Fas (CD95, DR2), TRAIL (Apo2L)/DR4 (TRAIL-R1) or DR5 (TRAIL-R2). When TNF-α binds to TNFR1, it recruits a protein called TNFR-associated death domain (TRADD) through its death domain (DD). TRADD then recruits a protein called Fas-associated protein with death domain (FADD), which then sequentially activates caspase-8 and caspase-3, and thus apoptosis. Alternatively, TNF-α can activate mitochondria to sequentially release ROS, cytochrome c, and Bax, leading to activation of caspase-9 and caspase-3 and thus apoptosis. Some of the miRNAs can inhibit apoptosis by targeting the death-receptor pathway including miR-21, miR-24, and miR-200c.

p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.

Some inhibitors of apoptosis proteins (IAPs) can inhibit apoptosis indirectly (such as cIAP1/BIRC2, cIAP2/BIRC3) or inhibit caspase directly, such as XIAP/BIRC4 (inhibits caspase-3, -7, -9), and Bruce/BIRC6 (inhibits caspase-3, -6, -7, -8, -9). 

Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases and malignancies especially cancer.

 

References:

1.Yağmur Kiraz, Aysun Adan, Melis Kartal Yandim, et al. Major apoptotic mechanisms and genes involved in apoptosis[J]. Tumor Biology, 2016, 37(7):8471.

2.Aggarwal B B, Gupta S C, Kim J H. Historical perspectives on tumor necrosis factor and its superfamily: 25 years later, a golden journey.[J]. Blood, 2012, 119(3):651.

3.Ashkenazi A, Fairbrother W J, Leverson J D, et al. From basic apoptosis discoveries to advanced selective BCL-2 family inhibitors[J]. Nature Reviews Drug Discovery, 2017.

4.McIlwain D R, Berger T, Mak T W. Caspase functions in cell death and disease[J]. Cold Spring Harbor perspectives in biology, 2013, 5(4): a008656.

5.Ola M S, Nawaz M, Ahsan H. Role of Bcl-2 family proteins and caspases in the regulation of apoptosis[J]. Molecular and cellular biochemistry, 2011, 351(1-2): 41-58.

Research Areas

Products Related to Apoptosis(3030)

  • GC81687 structure
    GC81687cis-V-11-0711
    CAS: 1428338-79-7
    Purity: >98%

    cis-V-11-0711 is the cis form of V-11-0711.

  • GC81690 structure
    GC81690BI1071
    Purity: >98.50%

    BI1071 is an orally active Nur77-Bcl-2 apoptotic pathway modulator.

  • GC81695 structure
    GC81695DIM-3,5-Cl2
    CAS: 2595179-74-9
    Purity: >99.00%

    DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with K D values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively.

  • GC81725 structure
    GC81725TRPV1 antagonist 10
    CAS: 896584-55-7
    Purity: >98.50%

    TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist ( IC 50 = 33.06 nM), moderate to weak URAT1 ( IC 50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor.

  • GC81754 structure
    GC81754(E)-FOBISIN101
    CAS: 1370281-06-3
    Purity: >95.50%

    (E)-FOBISIN101 is a 14-3-3 protein-protein interaction ( 14-3-3 protein-protein interaction ) inhibitor, with IC 50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively.

  • GC81757 structure
    GC817573-Ethoxy-5,6-dibromosalicylaldehyde
    CAS: 20041-64-9
    Purity: >99.50%

    3-Ethoxy-5,6-dibromosalicylaldehyde is an IRE1/ERN1 inhibitor, with an IC 50 of 0.12 μM, a K i of 71-88 nM, and a K d of 100 nM against the ribonuclease activity of hIRE1α, as well as an IC 50 of 4.8 μM against yeast Ire1.

  • GC81758 structure
    GC81758HDAC11-IN-5
    Purity: >98.00%

    HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC 50 of 0.021 μM.

  • GC81761 structure
    GC817614-Methoxycinnamic acid ethyl ester
    CAS: 1929-30-2
    Purity: >98.50%

    4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found.

  • GC81772 structure
    GC81772Epibestatin hydrochloride
    CAS: 100992-60-7
    Purity: >98.00%

    Epibestatin hydrochloride is an epimer of Bestatin, a DPP4 inhibitor and protease inhibitor, with an IC 50 of 17 μM against DPP4.

  • GC81818 structure
    GC8181811β,13-Dihydrolactucopicrin
    CAS: 125519-47-3
    Purity: >98%

    11β,13-Dihydrolactucopicrin is a sesquiterpene lactone and the main bitter component of chicory root.

  • GC81825 structure
    GC81825ASO-4625
    Purity: >98.00%

    ASO-4625 is a 20-nucleotide gapmer antisense oligonucleotide with a full phosphorothioate backbone and 2'-O-(2-methoxy) ethyl ribose modifications, which targets BCL2 mRNA and BCL2L1 mRNA.

  • GC81827 structure
    GC81827Buforin IIb TFA
    Purity: >98.00%

    Buforin IIb TFA (BF2-B TFA) is an anticancer peptide, as well as an Antibacterial and Antifungal agent.

  • GC81835 structure
    GC81835G4232
    Purity: >98.00%

    G4232 is an immune-silent BCL2 antisense oligonucleotide that binds to BCL2 mRNA to induce target degradation and inhibit Bcl-2 protein translation.

  • GC81843 structure
    GC81843Lumipodlin
    CAS: 2368183-94-0
    Purity: >98%

    Lumipodlin is a programmed cell death ligand 1 ( PD-L1 ) inhibitor.

  • GC81846 structure
    GC81846Nivitol
    CAS: 869743-37-3
    Purity: >98.00%

    Nivitol (UP302) is a natural phenolic compound discovered from Dianella ensifolia and also acts as a Tyrosinase inhibitor.

  • GC81850 structure
    GC81850p53 Bipartite NLS TFA
    Purity: >98.00%

    p53 Bipartite NLS TFA is a bipartite nuclear localization signal derived from p53.

  • GC81862 structure
    GC81862YJ1206 TFA
    Purity: >98.00%

    YJ1206 TFA is an orally active selective CDK12 / CDK13 PROTAC degrader.

  • GC81872 structure
    GC81872CPTH2-d₄
    Purity: >98%

    CPTH2 -d 4 is the deuterated-labeled CPTH2.

  • GC81873 structure
    GC81873Ciprofloxacin hydrochloride
    CAS: 86483-48-9
    Purity: >98.00%

    Ciprofloxacin hydrochloride (Bay-09867 hydrochloride) is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent.

  • GC81879 structure
    GC81879NCP26 TFA
    Purity: >99.50%

    NCP26 TFA is an ATP-competitive ProRS inhibitor (with a K D of 271 nM in the absence of proline, and a K D of 0.35 nM in the presence of 100 μM proline).

  • GC81880 structure
    GC81880OSU-2S TFA
    Purity: >98.00%

    OSU-2S TFA is a non-immunosuppressive derivative of Fingolimod hydrochloride (FTY720).

  • GC81890 structure
    GC81890Temozolomide-¹⁵N
    Purity: >98%

    Temozolomide - 15 N (NSC 362856- 15 N) is the 15 N-labeled Temozolomide.

  • GC81898 structure
    GC81898LLC355
    Purity: >99.50%

    LLC355 is a discoidin domain receptor 1 ( DDR1 ) ATTEC degrader with a DC 50 of 150.8 nM.

  • GC90076 structure
    GC90076HA-14-1
    CAS: 927635-64-1
    Purity: >95.00%

    Un inhibidor de Bcl-2